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Malaria kinase inhibitors
Infection

Academia/industry collaboration identifies antimalarials with new mechanism of action

April 2, 2024
Because of increasing resistance to current antimalarial drugs, new agents with novel mechanisms of action are needed. Plasmepsins are a family of 10 Plasmodium falciparum aspartic proteases (PMI to PMX), among which plasmepsins IX and X (PMIX and PMX) have been identified as potential targets due to their involvement in egress, invasion and parasite development.
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Immuno-oncology

Tetravalency of CTX-8371 achieves additional receptor occupancy and total target protein down-regulation

April 2, 2024
Researchers presented the development of a translational pharmacokinetic (PK)/receptor occupancy (RO) model of the tetravalent bispecific antibody (bsAb) CTX-8371 (Compass Therapeutics LLC) with the aim of investigating the possible effects of tetravalency compared to bivalency on RO and target internalization.
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3D illustration showing tumor inside prostate gland and closeup view of cancer cells
Cancer

DS-9300 targets epigenetic enzymes for prostate cancer

March 28, 2024
E1A binding protein (EP300) and CREB binding protein (CBP) are two closely related histone acetyltransferases (HATs), the mutations in which are related to several cancers. In the current study, researchers from Daiichi Sankyo Co. Ltd. aimed to develop orally available small molecule EP300/CBP HAT inhibitors with antitumor activity.
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Concept art for blood sugar.
Gastrointestinal

Fructose metabolism inhibitor shows promise for metabolic dysfunction

March 28, 2024
Ketohexokinase (KHK) is a sugar kinase that mediates fructose metabolism.
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Biomarkers

Proteomic identifiers of response to anti-PCSK9 biologics

March 28, 2024
Plasma pharmacodynamic biomarkers may be a reliable tool for biosimilarity assessment without having to rely on clinical trials, which are costly and time consuming.
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Cancer

YAP/pan-TEAD inhibitor has activity in Hippo-driven cancer models

March 28, 2024
Researchers from Merck & Co. Inc. have presented the discovery of inhibitors of the YAP/TAZ-TEAD complex as potential anticancer agents. YAP and its paralogue TAZ act as terminal effectors of the Hippo signaling pathway by regulating the transcriptional activity of the different TEAD isoforms.
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Malignant B-cell lymphocytes seen in Burkitt lymphoma, stained with hematoxylin and eosin (H&E) stain.
Cancer

SGR-1505, a MALT1 allosteric inhibitor with potent antitumor efficacy in models of B-cell lymphoma

March 27, 2024
Mucosa-associated lymphoid tissue lymphoma translocation protein 1 (MALT1) is a key regulator of physiological antigen receptor signaling in B cells and T cells, as it is the only component of the MALT1-BCL10-CARD11 (CBM) signalosome with proteolytic activity.
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Illustration of scientists conducting research on a mouse to find the missing puzzle piece
Neurology/Psychiatric

New murine models to study Clec7a in neurodegeneration

March 26, 2024
Microglia is known to play a crucial role in brain homeostasis, but this is lost during neurodegeneration.
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Skin irritation on hands
Dermatologic

GZ-21T reduces eczematous skin injury in preclinical atopic dermatitis

March 26, 2024
Atopic dermatitis (AD) is a chronic skin disease characterized by inflammation, barrier dysfunction, pruritus and eczematous lesions.
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Multiple myeloma illustration
Immuno-oncology

ORIC-533, a potent and selective CD73 inhibitor for cancer

March 26, 2024
Previous research has shown that adenosine impairs antitumor immunity, and high levels of adenosine and CD73 have been associated with poor prognosis in cancer.
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